Comparative Pharmacology
Head-to-head clinical analysis: PALIPERIDONE versus ZYPREXA RELPREVV.
Peer-Reviewed Evidence
Head-to-head clinical analysis: PALIPERIDONE versus ZYPREXA RELPREVV.
PALIPERIDONE vs ZYPREXA RELPREVV
Comparing the clinical profiles, pharmacokinetic behaviors, and safety indices of these two therapeutic agents.
Paliperidone is an atypical antipsychotic that exerts its effects primarily through antagonism of central dopamine D2 receptors and serotonin 5-HT2A receptors. It also antagonizes alpha-1 and alpha-2 adrenergic receptors, and H1 histaminergic receptors. Paliperidone is the major active metabolite of risperidone.
Olanzapine pamoate is a second-generation antipsychotic that antagonizes dopamine D2 and serotonin 5-HT2A receptors. It also binds to adrenergic α1, histamine H1, and muscarinic M1 receptors.
6 mg orally once daily, with dose adjustments in 3 mg increments at intervals of 5 days or more; usual effective range 3-12 mg/day.
210 mg intramuscular injection every 2 weeks; range 150-300 mg; max 300 mg per dose. For olanzapine-naive patients, establish tolerability with oral olanzapine before initiation.
None Documented
None Documented
Clinical Note
moderatePaliperidone + Levofloxacin
"Paliperidone may increase the QTc-prolonging activities of Levofloxacin."
Clinical Note
moderatePaliperidone + Norfloxacin
"Paliperidone may increase the QTc-prolonging activities of Norfloxacin."
Clinical Note
moderatePaliperidone + Gemifloxacin
"Paliperidone may increase the QTc-prolonging activities of Gemifloxacin."
Clinical Note
moderatePaliperidone + Fluticasone propionate
Approximately 23 hours for the extended-release oral formulation; provides steady trough concentrations with once-daily dosing
The terminal elimination half-life ranges from 30 to 60 days (mean ~45 days) after intramuscular injection, consistent with extended release from the depot formulation.
Renal (approximately 80% as unchanged drug and glucuronide conjugate), biliary/fecal (approximately 11%)
Approximately 57% of the dose is excreted in urine (30% as unchanged drug, 27% as metabolites) and 30% in feces (primarily as metabolites).
Category A/B
Category C
Atypical Antipsychotic
Atypical Antipsychotic
"The risk or severity of adverse effects can be increased when Paliperidone is combined with Fluticasone propionate."